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Loperimide

swybs said:
Sorry, the first ^^^ sentence I don't understand. What does that mean...

Also, at what dose does paralytic ileus typically occur? BTW, I'm not sure how opiate tolerance plays into this but my opiate tolerance wasn't extremely high; I was coming off approx 100mg oxy or equiv. daily with a 3 week clean period and 8 or so years of nonstop use, oftentimes at doses above 200mg.
swybs
Click to expand...


The first sentence means, how high is your specific Opioid-Tollerance on the MY-Receptors (the "normal" opiod tolerance", not the special opioid tolerance on DXM or PCP)

If you take 2 packages of Immodium om one time or you take half a package of it everyday for about two weeks, then you have the risk of an paralytic ileus...

But first you can have the symptoms of an "pseudo-ileus" (without the hardest of vomiting shit) - so I did..... Loperamide can accumulate in the fat-cells.... and could so be "uncalculatible"... If you get painful opstipation (you think you would pop), then it's time to quit...
 
I've used loperamide many times for withdrawal and it has never given me constipation. It just stops the diarrhea and some w/d symptoms. I've used up to 20mg with no harmful effects. I'm about to kick a 100mg OC habit and I plan on eating 40mg this time + xanax+ soma+ganja. This should really help with the withdrawals.
 
Immodium works great but only when you really need it. I had very severe flu about a month or two ago. Bearing in mind this flu was unrelenting, meant that every part of my body had to suffer - to the max. If you take it as directed it is like a life saver in these circumstances.
 
I think this abstract will help to understand why loperamide isn't centrally active:

Drug Dev Ind Pharm. 2004 May;30(5):449-59.

pH dependent uptake of loperamide across the gastrointestinal tract: an in vitro study.

Crowe A, Wong P.

School of Pharmacy, Curtin University of Technology, Perth, Western Australia. [email protected]

Loperamide is a peripherally acting antidiarrheal opioid with some affinity for P-glycoprotein (P-gp). One of the main reasons for its lack of central nervous system (CNS) activity is a combination first-pass metabolism and P-gp-mediated efflux preventing brain penetration. It was assumed that P-gp would also have a similar effect at the intestinal tract, limiting loperamide systemic absorption. However, previous in vitro studies had not determined loperamide flux using pH gradients present in the intestinal tract. Hence, our aim was to determine the influence of pH gradient conditions on the gastrointestinal uptake of loperamide, including any changes to its P-gp-mediated efflux. METHODS: Cellular uptake and transcellular transport were determined after exposure to various concentrations of loperamide (2-50 microM) with and without the presence of active efflux protein inhibitors. Loperamide was detected at 214 nm using high-performance liquid chromatography (HPLC) protocols. RESULTS: Bidirectional transport studies of 10 microM loperamide with a pH 6.0/7.4 apical (Ap)-to-basolateral (Bas) gradient showed efflux to be 17-fold higher than influx (10 ng/cm2/min Bas-->Ap compared to 0.6 for Ap-->Bas). This differential was much greater than when examined at pH 7.4/7.4 (only two-fold higher). The potent P-gp inhibitor, PSC-833, had only a moderate effect at blocking loperamide efflux under pH gradient conditions, yet could equilibrate bidirectional transport at pH 7.4. This suggested the presence of significant P-gp independent mechanisms, preventing loperamide access to the basolateral chamber. Amiloride and 5-(N-ethyl-N-isopropyl) amiloride had some effect on reducing efflux, hence the Na(+)--H(+) antiporter may have some involvement. Accumulation of loperamide into Caco-2 cells reduced almost 70% at pH 6.0 compared to pH 7.4, yet P-gp was always able to approximately double the equilibrium concentration in the cells within a defined pH study. This showed that P-gp was not affected by pH conditions. CONCLUSIONS: P-gp-mediated efflux of loperamide is supplemented under pH gradient conditions. Hence, drugs used to decrease acid secretion in the stomach could result in higher plasma loperamide levels based on our in vitro system reflecting the in vivo environment. The addition of a P-gp inhibitor could potentially further increase the gastrointestinal absorption of loperamide.

PMID: 15244080
 
It is now about 10 hours since my last small dose (10mg) of oxycontin. Usually in less then six hours I would be beginning to get sick, runny nose, anxiety, depression, restlessness, uncomfortable, unable to regulate body temperature, etc.

I ingested 30mg loperamide at about the five hour point along with 1mg of xanax, 1 cup of kava, and some cannabis. I feel fine. No real symptoms of w/d other then feeling very lethargic. This is coming from a five year on and off habit so my tolerance has been pretty high in the past. This time its off from a 100mg+ Oxy habit a day for several months. Not too bad, but definitely capable of producing 3-5 days of sickness.

I feel fine so far and I plan on taking some valerian+chamomile to help sleep tonight, as well as some more kava. I plan on taking less loperamide tomorrow until I can get down to a reasonable level to stop completely. hopefully I will be opiate free by my girlfriends spring break but I must guard against that dark lady in my dreams....
 
heady^^^, I think that is too high of a dose, in too short of a time...10 hours, and it shouldn't have WDs coming into full effects...though, you did say lessened dose (10mg). I would slow down and use them in dosages of 4-8 mg, intermittently throughout the day, when symptoms feel near (or show their ugly face--scratch that--ass)...

With the xanax and weed, you should be good. I wouldn't combine kava with high doses of loperamide, since kava is tough on the liver (and I am not sure of what doses you are using of kava).

The valerian should be fine for sleep; though I suspect the xanax, coupled with the smoke, should make you tired enough. Don't forget the unisom (or other equiv. OTC sleep aids--they really DO work).

Anyway, I did 100+ oxy WDs a few times and it wasn't that bad...though, it is all relative...have you gone through WDs many times before and how long was your longest clean period (to me, these factors seem to play into how long the WDs will last--I am now in my longest WD period in the past 9 years and I used most of the same drugs (both otc and others, including God's best WD medicine--subuxone)).

Anyway, good luck, and good luck with the dark lady--she is tough, especially watching your girlfriend have fun during spring break--ugg, dont I know how hard the easiest situations can now be, without the lady riding shotgun).

Anyway, keep us posted and slow down on the loperamide doses.

swybs
 
10mg was basically nothing, just enough to keep me from getting sick till about noon. The longest I have stayed clean in 5 years was 8 months. I'm always in for a good week of withdrawal after a solid month of use. It's amazing how quickly your tolerance returns even after an extended absence.

The kava is not too strong approximately 1000mg kalactones. I thought that the Kava liver problems was associated with not using the correct part of the plant? Also, do you think that the loperamide is hard on my liver? It doesn't feel toxic and I'm sure I'll have a bowel movement before I redose (20mg) tomorrow morning. I also take milk thistle daily and am not a heavy drinker.

Thanks for the info,

Heady
 
C6H6 said:
I think this abstract will help to understand why loperamide isn't centrally active:

Drug Dev Ind Pharm. 2004 May;30(5):449-59.

pH dependent uptake of loperamide across the gastrointestinal tract: an in vitro study.

Crowe A, Wong P.

School of Pharmacy, Curtin University of Technology, Perth, Western Australia. [email protected]

Loperamide is a peripherally acting antidiarrheal opioid with some affinity for P-glycoprotein (P-gp). One of the main reasons for its lack of central nervous system (CNS) activity is a combination first-pass metabolism and P-gp-mediated efflux preventing brain penetration. It was assumed that P-gp would also have a similar effect at the intestinal tract, limiting loperamide systemic absorption. However, previous in vitro studies had not determined loperamide flux using pH gradients present in the intestinal tract. Hence, our aim was to determine the influence of pH gradient conditions on the gastrointestinal uptake of loperamide, including any changes to its P-gp-mediated efflux. METHODS: Cellular uptake and transcellular transport were determined after exposure to various concentrations of loperamide (2-50 microM) with and without the presence of active efflux protein inhibitors. Loperamide was detected at 214 nm using high-performance liquid chromatography (HPLC) protocols. RESULTS: Bidirectional transport studies of 10 microM loperamide with a pH 6.0/7.4 apical (Ap)-to-basolateral (Bas) gradient showed efflux to be 17-fold higher than influx (10 ng/cm2/min Bas-->Ap compared to 0.6 for Ap-->Bas). This differential was much greater than when examined at pH 7.4/7.4 (only two-fold higher). The potent P-gp inhibitor, PSC-833, had only a moderate effect at blocking loperamide efflux under pH gradient conditions, yet could equilibrate bidirectional transport at pH 7.4. This suggested the presence of significant P-gp independent mechanisms, preventing loperamide access to the basolateral chamber. Amiloride and 5-(N-ethyl-N-isopropyl) amiloride had some effect on reducing efflux, hence the Na(+)--H(+) antiporter may have some involvement. Accumulation of loperamide into Caco-2 cells reduced almost 70% at pH 6.0 compared to pH 7.4, yet P-gp was always able to approximately double the equilibrium concentration in the cells within a defined pH study. This showed that P-gp was not affected by pH conditions. CONCLUSIONS: P-gp-mediated efflux of loperamide is supplemented under pH gradient conditions. Hence, drugs used to decrease acid secretion in the stomach could result in higher plasma loperamide levels based on our in vitro system reflecting the in vivo environment. The addition of a P-gp inhibitor could potentially further increase the gastrointestinal absorption of loperamide.

PMID: 15244080
Click to expand...

This post is very very interesting.... But it says exactly the opposite, what I had examined in about two dozend heavy loperamide-turns (which definitively where NOT placebo {e.g. I had a bigger miosis, in spite of the mydriasis from the quinine; and I had one time probs to breath {respiratory suppressions}}).

These turns got stronger, if I acidized the powder of the Immodium capsule with ascorbic-acid and I weakened the turns, if I alkalized the powder of the Immodium capsule with Natron (NaHCO³).

btw.: I haven't ingested the Immodium (oral). I applied the powder rhinal (snorted). Always exactly 1 hour after ingestion of 800 mg quinine. (But first I accumulated quinine with 800 mg on 3 days - as posted above)
 
What a great help loperamide has been for me! I only awoke once last night (2:30am) with minor "kicking", ate two more valerian pills and fell right back to sleep. This morning I didn't even need anything to get out of bed. I felt fine and even took a solid shit around noon. At about 2:00 I began to fill a little edgy so I took 15mg, half my previous dose, and now I feel fine again.

I would highly recommend buying a large bottle of loperamide tablets if you are facing cold turkey. I think my bottle was like $10 for 48 2mg tablets. Very helpful, cheap, convenient. I feel 90% when I would normally be going through hell, however it does nothing for the cravings.
 
loperamide shouldn't cross the blood brain barrier but , for some reason, when i took two of the chewable tablets (for it's constipative effects) i was very sleepy and could barely move for about two hours. weird...
 
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